PI-273 促销  ≥98%

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包装规格:5mg 10mg 25mg 50mg in glass bottle
溶解性:溶于DMSO(6.02 mg/mL 超声)
产品描述:基本信息 产品编号:P10810 产品名称:PI-273 CAS: 925069-34-7   储存条件 粉末 -20℃ 四年     分子式: C16H16ClN3O2S2 溶于液体 -80℃ 六个月 分子量 381.90 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.6185 mL 13.0924 mL 26.1849 mL 5mM 0.5237 mL 2.6185 mL 5.2370 mL 10mM 0.2618 mL 1.3092 mL 2.6185 mL   生物活性 产品描述 是第一种可逆的和特异性磷脂酰肌醇 4-激酶 (PI4KIIα) 抑制剂,IC50 为 0.47 μM。PI-273 可以抑制乳腺癌细胞的增殖,阻断细胞周期并诱导细胞凋亡。 靶点/IC50 YES Lyn Fyn Src   体外研究 PI-273 (2μM; 48 hours) blocks the cell cycle at the G2-M phase.PI-273 (2μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.PI-273 (0.5-2μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.PI-273 of 1μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner.PI-273 (2μM; 48 hours) blocks the cell cycle at the G2-M phase.PI-273 (2μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.PI-273 (0.5-2μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.PI-273 of 1μM and 2μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner. Cell Line: MCF-7, T-47D, SK-BR-3, MDA-MB-231, SUM229PE, Hs 578T cells Concentration: 2μM Incubation Time: 48 hours Result: Blocked the cell cycle at the G2-M phase. Apoptosis Analysis Cell Line: MCF-7, T-47D, and SK-BR-3 cells Concentration: 2μM Incubation Time: 48 hours Result: Induced cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SKBR-3. Western Blot Analysis Cell Line: MCF-7 cells Concentration: 0.5, 1, 2μM Incubation Time: For 3 days Result: Suppressed the AKT signaling pathway in a dose- and time-dependent manner. 体内研究 PI-273 (intraperitoneal injection; 25mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts.PI-273 (0.5mg/kg (intravenously) or 1.5mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%. Animal Model: Eight-week-old male BALB/c nude mice with MCF-7 cell Dosage: 25 mg/kg Administration: Intraperitoneal injection; daily; 15 days Result: Suppressed the tumor volume and weight in the MCF-7 xenografts.   Animal Model: Male Sprague-Dawley (SD) rats Dosage: 0.5mg/kg (intravenously) or 1.5mg/kg (intragastrically) (Pharmacokinetic Study) Administration: Intravenously or intragastrically; 0.08, 0.16, 0.33, 0.67, 1, 1.5, 2, 3 and 5 hours Result: Has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.
保存条件:-20℃